1. Cell Cycle/DNA Damage
    Apoptosis
  2. CDK
    Apoptosis
  3. Samuraciclib hydrochloride hydrate

Samuraciclib hydrochloride hydrate (Synonyms: CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate)

目录号: HY-103712B 纯度: 99.08% ee.: 99.88%
产品使用指南

Samuraciclib (CT7001) hydrochloride hydrate 是一种有效的,具有选择性,ATP 竞争性和口服活性的 CDK7 抑制剂,IC50 为 41 nM。Samuraciclib hydrochloride hydrate 对 CDK7 的选择性分别是 CDK1,CDK2 (IC50 为 578 nM),CDK5 和 CDK9 的 45 倍,15 倍,230 倍和 30 倍。Samuraciclib hydrochloride hydrate 以 GI50 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有有效的抗肿瘤作用。

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Samuraciclib hydrochloride hydrate Chemical Structure

Samuraciclib hydrochloride hydrate Chemical Structure

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2750
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5 mg ¥2500
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10 mg ¥4200
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25 mg ¥8600
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50 mg ¥14000
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  • 生物活性

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  • 参考文献

生物活性

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects[1][2].

IC50 & Target[1][2]

CDK7

41 nM (IC50)

CDK2

578 nM (IC50)

CDK1

1.8 μM (IC50)

CDK4

49 μM (IC50)

CDK5

9.4 μM (IC50)

CDK6

31 μM (IC50)

CDK9

1.2 μM (IC50)

体外研究
(In Vitro)

Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].
Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].
Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib trihydrochloride also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].
Samuraciclib (ICEC0942) hydrochloride hydrate inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 µM, 0.32 µM, 0. 33 µM, 0.21 µM, 0.22 µM, 0.67 µM and 1.25 µM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 24 hours
Result: Induced caspase 3/7 and demonstrated PARP cleavage.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.01 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 24 hours
Result: Showed accumulation of cells in G2/M.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.01 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 0 hour, 4 hours, 8 hours, 16 hours or 24 hours
Result: PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.
体内研究
(In Vivo)

Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) hydrochloride hydrate treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors[1].
The combination of Samuraciclib (ICEC0942) hydrochloride hydrate and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1]
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 14 days
Result: At day 14, tumor growth was inhibited by 60%.
Clinical Trial
分子量

521.70

Formula

C22H30N6O.(2.5HCl).(2H2O)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (191.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9168 mL 9.5841 mL 19.1681 mL
5 mM 0.3834 mL 1.9168 mL 3.8336 mL
10 mM 0.1917 mL 0.9584 mL 1.9168 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.79 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

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× = ×
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产品名称:
Samuraciclib hydrochloride hydrate
目录号:
HY-103712B
需求量: